Separated Solid-Liquid NSAID Composition for Transdermal Stability

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Solution Overview

Problem

Non-steroidal anti-inflammatory drugs (NSAIDs) cause adverse gastrointestinal reactions when administered orally, and existing derivatives for alternative routes like transdermal administration are not stable in solvent solutions.

Innovation Solution

A stable pharmaceutical composition is developed with a separated solid portion containing a pharmaceutically acceptable salt of a non-steroidal anti-inflammatory drug derivative and a separated liquid portion, using specific solvents, where the solid portion is stored separately to maintain stability and is formulated with a pharmaceutically acceptable binder to enhance dissolution and transdermal administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If non-steroidal anti-inflammatory drugs are administered orally, then therapeutic effects are achieved, but gastrointestinal adverse reactions occur

Engineering Contradiction:

Improvetherapeutic effectVSAvoidgastrointestinal adverse reactions

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The pharmaceutical composition is divided into separated solid portion and separated liquid portion, allowing the drug to be stored in solid form (avoiding GI irritation) and only dissolved when needed for transdermal application

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

A pharmaceutically acceptable binder is used as an intermediary to facilitate transdermal delivery of the NSAID derivative, enabling the drug to reach the systemic circulation through the skin rather than the gastrointestinal tract

Inventive Principle:

Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If NSAID derivatives are formulated in solvent solutions for transdermal administration, then gastrointestinal adverse reactions are avoided, but stability deteriorates

Engineering Contradiction:

Improvegastrointestinal adverse reactionsVSAvoiddrug stability

Core Design Contradiction:

Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The composition is segmented into solid drug portion and liquid solvent portion that are separated during storage, preventing degradation while enabling reconstitution for transdermal use

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The drug is maintained in solid state during storage and converted to solution state only when needed for application, changing the physical state parameter to maintain stability

Inventive Principle:

Principle #35Parameter changes

3Ease of operation

If NSAID derivatives are used for transdermal administration, then gastrointestinal adverse reactions are reduced, but stability in solvent solutions is poor

Engineering Contradiction:

Improvetransdermal administrationVSAvoidstability in solvent

Core Design Contradiction:

Ease of operationVSStability of the object's composition

Solution Approach 1:

The composition separates the drug substance (solid) from the solvent (liquid), maintaining stability during storage while enabling transdermal administration when mixed

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The pharmaceutical composition uses a composite approach combining solid drug portion with pharmaceutically acceptable binder and liquid portion with solvent, creating a stable system that enables transdermal delivery

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS12403117B2Stable pharmaceutical composition containing non-steroidal anti-inflammatory drug derivative

Publication Date: 2025.09.02 ZHEJIANG YUEYA PHARMA CO LTD

AI summary

A stable pharmaceutical composition containing a non-steroidal anti-inflammatory drug derivative, at least comprising a separated solid part and liquid part, the solid part comprising a therapeutically effective dose of non-steroidal anti-inflammatory drug derivative and the liquid part being a pharmaceutically acceptable solvent. After a long-term stability study (25° C.±2° C., 12 months), the stability of the solid part was good, and met the requirements of the pharmaceutical industry.